Embusartan

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MedKoo CAT#: 525004

CAS#: 156001-18-2

Description: Embusartan, also known as BAY 10-6734, is a potent, orally active angiotensin II receptor antagonist being developed by Bayer as an antihypertensive agent. The compound has potential for once daily administration with antihypertensive activity still present over a 24-h period. Embusartan was under preclinical development in Germany for the treatment of hypertension.

Chemical Structure

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Embusartan
CAS# 156001-18-2
Instruction

Theoretical Analysis

MedKoo Cat#: 525004
Name: Embusartan
CAS#: 156001-18-2
Chemical Formula: C25H24FN5O3
Exact Mass: 461.19
Molecular Weight: 461.490
Elemental Analysis: C, 65.07; H, 5.24; F, 4.12; N, 15.18; O, 10.40

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: Embusartan; Bay 10-6734; Embusartan [INN]; UNII-4MY73645XA.

IUPAC/Chemical Name: 6-n-Butyl-4-methoxycarbonyl-2-oxo-1-((2'-(1H-tetrazol-5-yl)-3-fluorobiphenyl-4-yl)methyl)-1,2-dihydropyridine

InChi Key: LYVGOAYMIAQLHI-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H24FN5O3/c1-3-4-7-19-12-18(25(33)34-2)14-23(32)31(19)15-17-11-10-16(13-22(17)26)20-8-5-6-9-21(20)24-27-29-30-28-24/h5-6,8-14H,3-4,7,15H2,1-2H3,(H,27,28,29,30)

SMILES Code: CCCCc1cc(cc(=O)n1Cc2ccc(cc2F)c3ccccc3c4[nH]nnn4)C(=O)OC

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 461.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Wang JM, Tan J, Leenen FH. Central nervous system blockade by peripheral administration of AT1 receptor blockers. J Cardiovasc Pharmacol. 2003 Apr;41(4):593-9. PubMed PMID: 12658061.

2: Balt JC, Mathy MJ, Pfaffendorf M, van Zwieten PA. Sympatho-inhibitory properties of various AT1 receptor antagonists. J Hypertens Suppl. 2002 Jun;20(5):S3-11. PubMed PMID: 12184061.

3: Balt JC, Mathy MJ, Pfaffendorf M, van Zwieten PA. Inhibition of facilitation of sympathetic neurotransmission and angiotensin II-induced pressor effects in the pithed rat: comparison between valsartan, candesartan, eprosartan and embusartan. J Hypertens. 2001 Dec;19(12):2241-50. PubMed PMID: 11725169.

4: Zhang J, Leenen FH. Peripheral administration of AT1 receptor blockers and pressor responses to central angiotensin II and sodium. Can J Physiol Pharmacol. 2001 Oct;79(10):861-7. Erratum in: Can J Physiol Pharmacol 2001 Dec;79(12):1045. PubMed PMID: 11697745.

5: Zhang J, Leenen FH. AT(1) receptor blockers prevent sympathetic hyperactivity and hypertension by chronic ouabain and hypertonic saline. Am J Physiol Heart Circ Physiol. 2001 Mar;280(3):H1318-23. PubMed PMID: 11179079.

6: Warnholtz A, Nickenig G, Schulz E, Macharzina R, Bräsen JH, Skatchkov M, Heitzer T, Stasch JP, Griendling KK, Harrison DG, Böhm M, Meinertz T, Münzel T. Increased NADH-oxidase-mediated superoxide production in the early stages of atherosclerosis: evidence for involvement of the renin-angiotensin system. Circulation. 1999 Apr 20;99(15):2027-33. PubMed PMID: 10209008.

7: Iouzalen L, Stepien O, Marche P. Effects of BAY 10-6734 (Embusartan), a new angiotensin II type I receptor antagonist, on vascular smooth muscle cell growth. J Pharmacol Exp Ther. 1999 Apr;289(1):181-7. PubMed PMID: 10087002.

8: Böhm M, Zolk O, Flesch M, Schiffer F, Schnabel P, Stasch JP, Knorr A. Effects of angiotensin II type 1 receptor blockade and angiotensin-converting enzyme inhibition on cardiac beta-adrenergic signal transduction. Hypertension. 1998 Mar;31(3):747-54. PubMed PMID: 9495257.

9: Breithaupt-Grögler K, Malerczyk C, Belz GG, Butzer R, Herrmann V, Stass H, Wensing G. Pharmacodynamic and pharmacokinetic properties of an angiotensin II receptor antagonist--characterization by use of Schild regression technique in man. Int J Clin Pharmacol Ther. 1997 Oct;35(10):434-41. PubMed PMID: 9352392.

10: Stasch JP, Knorr A, Hirth-Dietrich C, Krämer T, Hübsch W, Dressel J, Fey P, Beuck M, Sander E, Frobel K, Kazda S. Long-term blockade of the angiotensin II receptor in renin transgenic rats, salt-loaded Dahl rats, and stroke-prone spontaneously hypertensive rats. Arzneimittelforschung. 1997 Sep;47(9):1016-23. PubMed PMID: 9342414.

11: Flesch M, Schiffer F, Zolk O, Pinto Y, Stasch JP, Knorr A, Ettelbrück S, Böhm M. Angiotensin receptor antagonism and angiotensin converting enzyme inhibition improve diastolic dysfunction and Ca(2+)-ATPase expression in the sarcoplasmic reticulum in hypertensive cardiomyopathy. J Hypertens. 1997 Sep;15(9):1001-9. PubMed PMID: 9321748.